N-(2-(4'-cyanobiphenyl-4-yl)propyl)propane-2-sulfonaMide
N-(2-(4'-cyanobiphenyl-4-yl)propyl)propane-2-sulfonaMide Basic information
- Product Name:
- N-(2-(4'-cyanobiphenyl-4-yl)propyl)propane-2-sulfonaMide
- Synonyms:
-
- LY404187
- N-(2-(4'-Cyano-[1,1'-biphenyl]-4-yl)propyl)propane-2-sulfonaMide
- N-[2-(4'-Cyano[1,1'-biphenyl]-4-yl)propyl]-2-propanesulfonamide
- N-2-(4-(4-Cyanophenyl)phenyl)propyl-2-propanesulfonamide
- CS-2739
- 100775
- LY-404187; LY 404187
- LY-404187 N-(2-(4'-cyanobiphenyl-4-yl)propyl)propane-2-sulfonaMide
- CAS:
- 211311-95-4
- MF:
- C19H22N2O2S
- MW:
- 342.46
- Mol File:
- 211311-95-4.mol
N-(2-(4'-cyanobiphenyl-4-yl)propyl)propane-2-sulfonaMide Chemical Properties
- Boiling point:
- 519.0±60.0 °C(Predicted)
- Density
- 1.19±0.1 g/cm3(Predicted)
- storage temp.
- Sealed in dry,Room Temperature
- solubility
- DMF: 15mg/mL; DMSO: 15mg/mL; DMSO:PBS (pH 7.2) (1:4): 0.2mg/mL; Ethanol: 3mg/mL
- form
- A solid
- pka
- 11.24±0.40(Predicted)
- color
- White to off-white
N-(2-(4'-cyanobiphenyl-4-yl)propyl)propane-2-sulfonaMide Usage And Synthesis
Description
LY404187 is a benzothiadiazide positive allosteric modulator of AMPA receptors. It increases glutamate-induced activation of GluR1i, -2i, -2o, -3i, and -4i subunit-containing AMPA receptors with EC50 values of 5.65, 0.15, 1.44, 1.66, and 0.21 μM, respectively, in a calcium influx assay. LY404187 is selective for these AMPA receptors over GluR6 subunit-containing kainate receptors at 10 μM. LY404187 increases currents induced by glutamate and AMPA in rat prefrontal cortex pyramidal neurons (EC50s = 1.3 and 1.2 μM, respectively) but not in AMPA-stimulated primary rat embryonic hippocampal or primary cerebellar Purkinje neurons. LY404187 prevents decreases in the number of dopaminergic neurons in the substantia nigra induced by MPTP and 6-OHDA in mouse and rat, respectively, models of Parkinson’s disease when administered at a dose of 0.5 mg/kg per day.
Uses
LY 404187 is a novel positive allosteric modulator of AMPA receptors.
in vivo
LY-404187 (0.5 mg/kg; s.c for 11 days) can prevent MPTP-induced neurotoxicity in mice[4].
LY-404187 (0.5 mg/kg; s.c. for 28 days) attenuates apomorphine-induced contraversive rotations and affords significant protection against the loss of tyrosine hydroxylase positive nigral cell bodies[4].
LY-404187 (0.1 or 0.5 mg/kg; s.c. for 14 days) affords functional, neurochemical and histological protection after infusion of 6-hydroxydopamine into the substantia nigra in rats[4].
LY-404187 (0.5 mg/kg; s.c. for 14 days) delayed treatment provides functional and histological improvement, suggesting a trophic action as administration is initiated after cell death[4].
LY-404187 (0.1 and 0.5 mg/kg; s.c. for 14 days) increases GAP-43 immunoreactivity in the striatum in a dose-dependent manner[4].
Animal Model: | Male C57BL/6J mice (20-25 g) are challenged with MPTP on day 8[4] |
Dosage: | 0.5 mg/kg |
Administration: | S.c; twice daily on weekdays and once daily at weekends for 11 days |
Result: | Attenuated the loss of tyrosine hydroxylase immunoreactivity in the substantia nigra. No significant change in tyrosine hydroxylase immunoreactivity in the dorsal and ventral striatum. |
storage
Store at +4°C
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